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5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2016-10-28 21:43:49
Wenlin Huang, Matthew A. Hulverson, Zhongsheng Zhang, Ryan Choi, Kevin J. Hart, Mark Kennedy, Rama Subba Rao Vidadala, Dustin J. Maly, Wesley C. Van Voorhis, Scott E. Lindner, Erkang Fan, Kayode K. Ojo

Plasmodium falciparum calcium-dependent protein kinase 4 (PfCDPK4) is essential for the exflagellation of male gametocytes. Inhibition of PfCDPK4 is an effective way of blocking the transmission of malaria by mosquitoes. A series of 5-aminopyrazole-4-carboxamide analogues are demonstrated to be potent inhibitors of PfCDPK4. The compounds are also able to block exflagellation of Plasmodium falciparum male gametocytes without observable toxicity to mammalian cells.

中文翻译:

5-Aminopyrazole-4-Carboxamide类似物是恶性疟原虫微配子细胞外排和潜在疟疾传播阻断剂的选择性抑制剂

恶性疟原虫钙依赖性蛋白激酶4(PfCDPK4)对雄性配子细胞的外分泌至关重要。抑制PfCDPK4是阻止蚊子传播疟疾的有效方法。一系列5-氨基吡唑-4-羧酰胺类似物被证明是PfCDPK4的有效抑制剂。该化合物还能够阻止恶性疟原虫雄配子细胞的释放,而对哺乳动物细胞没有可观察到的毒性。
更新日期:2016-10-29
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